217172-23-1Relevant academic research and scientific papers
Structure-activity relationship of N-methyl-N-aralkylpeptidylamines as novel N-type calcium channel blockers
Hu, Lain-Yen,Ryder, Todd R.,Rafferty, Michael F.,Dooley, David J.,Geer, Joann J.,Lotarski, Susan M.,Miljanich, George P.,Millerman, Elizabeth,Rock, David M.,Stoehr, Sally J.,Szoke, Balazs G.,Taylor, Charles P.,Vartanian, Mark G.
, p. 2151 - 2156 (1999)
Selective N-type voltage sensitive calcium channel (VSCC) blockers have shown efficacy in several animal models of stroke and pain. In the process of searching for small molecule N-type calcium channel blockers, we have identified a series of N-methyl-N-aralkyl-peptidylamines with potent functional activity at N-type VSCCs. The most active compound discovered in this series is PD 173212 (11, IC50 = 36 nM in the IMR32 assays). SAR and pharmacological evaluation of this series are described.
Peptidyl calcium channel blockers
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, (2008/06/13)
The present invention provides compounds that block calcium channels having the Formula I shown below. The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.
Reduced dipeptide analogues as calcium channel antagonists
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, (2008/06/13)
The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma. The nov
TYROSINE-DERIVED COMPOUNDS AS CALCIUM CHANNEL ANTAGONISTS
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, (2008/06/13)
The present invention provides compounds that block calcium channels and have the Formula I: and pharmaceutically acceptable salts, esters, and pro-drugs thereof, whereinR 1 and R 2 are independently H, phenylcyclopentylcarbonyl, C 1-C 7 alkyl, cyclohexyl
Heteroaryl alkyl alpha substituted peptidylamine calcium channel blockers
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, (2008/06/13)
The present invention provides compounds that block calcium channels having the Formula I shown below. The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, asthma, amyotropic lateral sclerosis, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.
Substituted peptidylamine calcium channel blockers
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, (2008/06/13)
PCT No. PCT/US98/10838 Sec. 371 Date Jan. 19, 1999 Sec. 102(e) Date Jan. 19, 1999 PCT Filed May 28, 1998 PCT Pub. No. WO98/54123 PCT Pub. Date Dec. 3, 1998The present invention provides compounds that block calcium channels having the Formula I shown belo
